LenalidoMide

Lenalidomide is a potent immunomodulatory agent that inhibits the secretion of pro‑inflammatory cytokines and increases the secretion of anti‑inflammatory cytokines from peripheral blood mononuclear cells. As a thalidomide analogue, Lenalidomide exerts its cellular activities through its target cereblon, a component of the cullin‑RING E3 ubiquitin ligase enzyme complex. The compound is more soluble in organic solvents and low pH solutions compared to thalidomide, offering improved pharmaceutical properties. Lenalidomide is also a valuable building block for constructing small molecules for targeted protein degradation and PROTAC (proteolysis‑targeting chimeras) technology. As a high‑purity reference standard, Lenalidomide is indispensable for analytical method development, impurity profiling, quality control testing, and ANDA filings for generic lenalidomide manufacturers. Additionally, Lenalidomide serves as a critical tool compound for studying immunomodulation, cereblon biology, and developing novel targeted protein degradation therapies.

 

Product Parameters

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Parameter	Specification
Product Name	Lenalidomide
CAS Number	191732-72-6
Molecular Formula	C₁₃H₁₃N₃O₃
Molecular Weight	259.26 g/mol
Physical Form	Solid
Appearance	Yellow solid
Melting Point	265268°C
Boiling Point	614.0±55.0°C (Predicted)
Density	1.460±0.06 g/cm³ (Predicted)
pKa	10.75±0.40 (Predicted)
Solubility	DMSO: up to 30 mg/mL
Storage Condition	28°C

Mechanism Of Action

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Lenalidomide is an immunomodulatory drug with multiple mechanisms of action. In vitro studies have demonstrated three primary effects of lenalidomide: 1) direct antitumor activity; 2) inhibition of angiogenesis; and 3) immunomodulatory effects. In vivo, lenalidomide induces apoptosis of tumor cells directly or indirectly by suppressing support from bone marrow stromal cells, inhibiting angiogenesis and osteoclast activity, and exerting immunomodulatory effects. At the molecular level, lenalidomide has been shown to interact with ubiquitin E3 ligase and target this enzyme to degrade the Ikaros transcription factors IKZF1 and IKZF3.

 

Bioactivity

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Lenalidomide (CC-5013) is a TNF-α secretion inhibitor with an IC50 of 13 nM in PBMCs. It serves as a ligand for ubiquitin E3 ligase cerebrolon (CRBN), inducing selective ubiquitination and degradation of the two lymphoid transcription factors IKZF1 and IKZF3 via CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes the expression of cleaved caspase-3, inhibits VEGF expression, and induces apoptosis.

 

Antitumor Drug

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Lenalidomide is an antitumor drug developed by Celgene Inc., a biopharmaceutical company based in the United States. Its chemical structure resembles that of thalidomide, and it exhibits multiple therapeutic effects including antitumor activity, immunomodulation, and antiangiogenesis. It inhibits the secretion of pro-inflammatory cytokines and enhances the production of anti-inflammatory cytokines by peripheral blood monocytes. In vitro studies have demonstrated its ability to suppress proliferation in certain cell lines, such as Namalwa cells. Lenalidomide also inhibits the growth of both patient-derived multiple myeloma cells and MM1S cells. Additionally, it reduces the expression of cyclooxygenase 2 (COX-2) but shows no effect on COX-1. Two multicenter, randomized, blinded, placebo-controlled clinical trials evaluated the safety and efficacy of lenalidomide in treating multiple myeloma, with disease progression time (TTP) serving as the primary efficacy endpoint. Interim analyses revealed that the combination therapy group exhibited significantly better TTP compared to the dexamethasone monotherapy group. Recent clinical studies further indicate that lenalidomide is effective not only in treating myelodysplastic syndromes (MDS) and multiple myeloma but also in managing myeloma, leukemia, metastatic renal carcinoma, solid tumors, primary systemic amyloidosis, and systemic myelofibrosis with myeloid metaplasia.

 

Lenalidomide is a next-generation derivative of thalidomide, yet no teratogenic toxicity has been observed, and its efficacy is 100 times stronger than that of thalidomide. According to Phase III clinical trial results, lenalidomide is currently the most effective drug for treating multiple myeloma, with over half of patients experiencing survival extension exceeding three years after treatment. Additionally, it is the only medication capable of effectively treating myelodysplastic syndrome (MDS); clinical data indicate that 64% of MDS patients require no further blood transfusions following lenalidomide therapy.

 

In December 2005, the U.S. Food and Drug Administration (FDA) approved lenalidomide for the treatment of myelodysplastic syndrome (MDS).

 

In March 2006, the FDA approved lenalidomide, manufactured by U.S.-based Celgene Biopharmaceuticals, for the treatment of multiple myeloma (MM).

 

On September 23,2011, the European Medicines Agency (EMA) issued a statement confirming that lenalidomide (brand name: Revlimid) demonstrated a benefit outweighing risk in its approved patient population, while simultaneously warning physicians about the potential risk of inducing new-onset cancer. Lenalidomide was administered in combination with dexamethasone for adult patients with multiple myeloma who had received at least one prior treatment. Three new studies demonstrated an increased incidence of new-onset cancer in patients with newly diagnosed multiple myeloma receiving lenalidomide alongside other combination therapies.

 

Contact Us

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For Lenalidomide with guaranteed quality, full traceability, and regulatory‑ready documentation, Cosperpharm is your trusted partner — contact us today.